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Design and structure-activity relationship analysis of ligands of gamma-hydroxybutyric acid receptors

✍ Scribed by Jean-Jacques Bourguignon; Martine Schmitt; Bruno Didier

Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
263 KB
Volume
20
Category
Article
ISSN
0741-8329

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✦ Synopsis

With the use of [ 3 H]gamma-hydroxybutyric acid, binding experiments allowed the screening of new compounds as ligands of gammahydroxybutyric acid receptors. Starting from the acid-alcohol gamma-hydroxybutyric acid structure, structure-activity relation analysis and lead optimization highlighted gamma-hydroxybutyric acid derivatives with significantly increased affinities, when compared with the affinity of gamma-hydroxybutyric acid. Further pharmacological studies with the use of gamma-hydroxybutyric acid derivatives allowed the characterization of the first competitive antagonist acting at gamma-hydroxybutyric acid receptors (NCS 382).

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